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Molecules 2015, 20(6), 9496-9509;

Enhanced Supersaturation and Oral Absorption of Sirolimus Using an Amorphous Solid Dispersion Based on Eudragit® E

College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea
College of Pharmacy, Pusan National University, Busan 609-735, Korea
College of Pharmacy, Kyungsung University, Busan 608-736, Korea
College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 406-840, Korea
Authors to whom correspondence should be addressed.
Academic Editors: Thomas Rades, Holger Grohganz and Korbinian Löbmann
Received: 10 April 2015 / Accepted: 20 May 2015 / Published: 25 May 2015
(This article belongs to the Collection Poorly Soluble Drugs)
Full-Text   |   PDF [2647 KB, uploaded 25 May 2015]   |  


The present study aimed to investigate the effect of Eudragit® E/HCl (E-SD) on the degradation of sirolimus in simulated gastric fluid (pH 1.2) and to develop a new oral formulation of sirolimus using E-SD solid dispersions to enhance oral bioavailability. Sirolimus-loaded solid dispersions were fabricated by a spray drying process. A kinetic solubility test demonstrated that the sirolimus/E-SD/TPGS (1/8/1) solid dispersion had a maximum solubility of 196.7 μg/mL within 0.5 h that gradually decreased to 173.4 μg/mL after 12 h. According to the dissolution study, the most suitable formulation was the sirolimus/E-SD/TPGS (1/8/1) solid dispersion in simulated gastric fluid (pH 1.2), owing to enhanced stability and degree of supersaturation of E-SD and TPGS. Furthermore, pharmacokinetic studies in rats indicated that compared to the physical mixture and sirolimus/HPMC/TPGS (1/8/1) solid dispersion, the sirolimus/E-SD/TPGS (1/8/1) solid dispersion significantly improved oral absorption of sirolimus. E-SD significantly inhibited the degradation of sirolimus in a dose-dependent manner. E-SD also significantly inhibited the precipitation of sirolimus compared to hydroxypropylmethyl cellulose (HPMC). Therefore, the results from the present study suggest that the sirolimus-loaded E-SD/TPGS solid dispersion has great potential in clinical applications. View Full-Text
Keywords: sirolimus; supersaturation; bioavailability; Eudragit® E; solid dispersion sirolimus; supersaturation; bioavailability; Eudragit® E; solid dispersion

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Cho, Y.; Ha, E.-S.; Baek, I.-H.; Kim, M.-S.; Cho, C.-W.; Hwang, S.-J. Enhanced Supersaturation and Oral Absorption of Sirolimus Using an Amorphous Solid Dispersion Based on Eudragit® E. Molecules 2015, 20, 9496-9509.

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